PNU-177864
CAS No. : 250266-51-4
| Size | Price | Stock |
|---|---|---|
| 5mg | $200 | In-stock |
| 10mg | $290 | In-stock |
| 25mg | $590 | In-stock |
| 50mg | $830 | In-stock |
| 100mg | $1150 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-103406 |
| M.Wt: | 402.43 |
| Formula: | C18H21F3N2O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 57.14 mg/mL (adjust pH to 5 with HCL) |
PNU-177864 is a potent, selective, orally active dopamine D3 receptor antagonist. PNU-177864 induces phospholipid metabolism in vivo and has anti-schizophrenia activity[1][2][3].
In Vitro:PNU-177864 (1-10 μM, 30 min) reduces CCR5 expression in THP1, reduces inflammation[1].
In Vivo:PNU-177864 (0-200 mg/kg,p.o., once daily for 2 weeks) can cause significant phospholipidosis and associated myopathy under certain conditions in rats, with plasma levels increasing throughout 24 hours at high doses. It remains high and almost unchanged over the dosing interval, but it has no obvious toxicity at lower doses[2].
PNU-177864 (0-200 mg/kg, p.o., once daily for 2 weeks) in rats and dogs is the accumulation of phospholipids in epididymal epithelial cells[3].
Pharmacokinetic analysis of oral PNU-177864 in rats[2]
| Treatment (mg/kg/day) | Day | Cmax (μg/mL) | Tmax (h) | C24 (μg/mL) | t1/2 (h) | AUC0-24 (μg•h/mL) | AUC0-∞ (ng•h/mL) |
| 12.5 | 1 | 0.88 | 4-8 | 0.167 | 6.5 | 13.2 | 15.1 |
| 12.5 | 6 | nc | nc | 0.23 | nc | nc | nc |
| 12.5 | 14 | 1.25 | 2-8 | 0.237 | 7.1 | 18.4 | nc |
| 50 | 1 | 3.64 | 8 | 1.84 | 16 | 63.9 | 117 |
| 50 | 6 | nc | nc | 2.74 | nc | nc | nc |
| 50 | 14 | 5.7 | 4-8 | 2.50 | 13.7 | 104 | nc |
| 200 | 1 | 6.9 | 8-24 | 6.8 | / | 133 | nc |
| 200 | 6 | nc | nc | 14.3 | nc | nc | nc |
| 200 | 11 | 15.9 | 0-8 | 11.06 | / | 306 | nc |